Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Kurt W. Saionz"'
Autor:
Hunmin Jung, Kyu Y. Rhee, Mi-Sun Koo, Michael J. Szymonifka, Reiling Liao, Tige R. Rustad, Molly R Nixon, Kurt W. Saionz, Anuradha Kumar, David R. Sherman, James C. Sacchettini, Joel S. Freundlich, Madhumitha Nandakumar, Justin P. Roberts
Publikováno v:
Chemistry & Biology. 21(7):819-830
Summary In this study, we identified antifolates with potent, targeted activity against whole-cell Mycobacterium tuberculosis (MTB). Liquid chromatography-mass spectrometry analysis of antifolate-treated cultures revealed metabolic disruption, includ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed713cc3675c688ce288c42f1eb6b4b5
Publikováno v:
Tetrahedron Letters. 52:849-852
A synthesis of novel substituted 3,8,11-triazaspiro[5,6]dodecan-7-ones using a combination of solution-phase and solid-phase chemistries is described. A solution-phase approach was used to produce a key piperidine intermediate that was then incorpora
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f245d43a2ed805654a8e49cd62337ea4
https://doi.org/10.1016/j.tetlet.2010.11.150
https://doi.org/10.1016/j.tetlet.2010.11.150
Autor:
W. Lynn Rogers, Brian F. Mcguinness, Kurt W. Saionz, Steven G. Kultgen, Vikash Srivastava, Hema Desai, Hao Yan, Tara M. Stauffer, Samiran Saha, Koc-Kan Ho, Shengting Zhang, Neelima Mannava, Yan Jiang, Anthony E. Klon, Tailong Li, Juxing Yin, Weiqing Chen, Konghua Jing, Maria L. Webb, Kanak Kanti Majumdar, Laura L. Rokosz
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7414-7420
A novel series of quinolinone-based adenosine A2B receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted essential structural features
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3954d9929bb24932679a9f1fdf525fd0
https://doi.org/10.1016/j.bmcl.2010.10.030
https://doi.org/10.1016/j.bmcl.2010.10.030
Autor:
Lan-Ying Qin, Kurt W. Saionz, Roland E. Dolle, Baldwin John J, Marc-Raleigh Brescia, Joan J. Zhang, James R. Wareing, Ian R. Henderson, Juerg Zimmermann, Axel Metzger, Pascal Rigollier, Hubert Gstach, Andrew G. Cole
Publikováno v:
Tetrahedron Letters. 51:4486-4489
A facile synthesis of novel 2-amino-6-arylmethyl-7-carboxamido-7,8-dihydropyrimido[5,4-f][1,4]thiazepin-5-ones is described. The synthesis was developed on solid phase and was applied to provide a series of analogs in good yield. The key reactions ar
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::612c6229b945ede53f82e56c7f50e463
https://doi.org/10.1016/j.tetlet.2010.06.070
https://doi.org/10.1016/j.tetlet.2010.06.070
Autor:
Hubert Gstach, Andrew G. Cole, Ian R. Henderson, Baldwin John J, Juerg Zimmermann, Roland E. Dolle, Lan-Ying Qin, James R. Wareing, Wolfgang K.-D. Brill, Axel Metzger, Kurt W. Saionz, Marc-Raleigh Brescia
Publikováno v:
Tetrahedron Letters. 50:7082-7085
An efficient and general synthesis of substituted 2-amino-7,8-dihydropteridin-6(5H)-ones using a combination of solution-phase and solid-phase chemistry is described. Solution-phase chemistry was used to produce two pyrimidine regioisomers that were
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::226ff5b78225e18bf164076aa818b1f5
https://doi.org/10.1016/j.tetlet.2009.10.005
https://doi.org/10.1016/j.tetlet.2009.10.005
Autor:
Babu Suresh D, R. Kuvelkar, Yuhua Huang, A.W. Stamford, Qi Zhang, Lili Zhang, P. Gaspari, J. Pan, Wang Lingyan, L. Ozgur, Ge Li, Yusheng Wu, Johannes H. Voigt, Xiao Chen, Kurt W. Saionz, J. Lowrie, Tao Guo, Ulrich Iserloh, N.A. McHugh, D. Tadesse, Le Thuy X H, Matthew E. Kennedy, Doug W. Hobbs, Leonard Favreau, Carolyn DiIanni Carroll, Corey Strickland, Jared N. Cumming, Eric M. Parker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3236-3241
Guided by structure-based design, we synthesized two novel series of potent inhibitors of BACE1 and generated extensive SAR around both the prime and non-prime side binding pockets. The key feature of both series is a cyclic amine motif specifically
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6ecdbdfa7bbf11174961bb58e02315b3
https://doi.org/10.1016/j.bmcl.2008.04.050
https://doi.org/10.1016/j.bmcl.2008.04.050
Autor:
Damian Arnaiz, Gary Phillips, Shawn David Erickson, Marc Whitlow, Margaret Kenrick, James J. Devlin, Gonghua Pan, Cecile Santos, William J. Guilford, Robert G. Wei, Marc Adler, Kurt W. Saionz, Bin Ye, Ron Vergona, John Parkinson, Zuchun Spring Zhao, David D. Davey, Michael Ohlmeyer, Babu Subramanyam, Vidyadhar M. Paradkar, Mark A. Polokoff, Keith A. Eagen, Michael M. Morrissey
Publikováno v:
Journal of Medicinal Chemistry. 50:1146-1157
By the screening of a combinatorial library for inhibitors of nitric oxide (NO) formation by the inducible isoform of nitric oxide synthase (iNOS) using a whole-cell assay, 2-(imidazol-1-yl)pyrimidines were identified. Compounds were found to inhibit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4d006ce8377fe93f50d8103040b4acb
https://doi.org/10.1021/jm061319i
https://doi.org/10.1021/jm061319i
Autor:
Zahid Hussain, Baldwin John J, Tohru Takashi, Kurt W. Saionz, K.J.M. Moriarty, Mika Yokoyama, Edward Mcdonald, Sarko Christopher Ronald, Nobuo Machinaga, Angela Wong, Atsushi Nakayama, Jun Chiba, Gensuke Takayama, Robert Swanson
Publikováno v:
Bioorganic & Medicinal Chemistry. 14:2725-2746
A series of prolyl-1-piperazinylacetic acid and prolyl-4-piperidinylacetic acid derivatives were synthesized and evaluated for their activity as VLA-4 antagonists. Of 22 compounds synthesized, 19 compounds showed potent activity with low nanomolar IC
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd40127b92d08dffc9405bdddf9ef894
https://doi.org/10.1016/j.bmc.2005.11.058
https://doi.org/10.1016/j.bmc.2005.11.058
Autor:
Kenneth J. Valenzano, Kurt W. Saionz, Ruiyan Liu, Dan Xie, Koc-Kan Ho, Edward Mcdonald, Guizhen Dong, Steven G. Kultgen, Peng Geng, Tao Guo, Dan Fitzpatrick, Roland E. Dolle, Anton E.P. Adang, Nicole C.R. van Straten, Brian F. Mcguinness, Maria L. Webb
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1713-1716
High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC50=3 μM) and 2 (EC50=3.9 μM), based on which a focused combinatoria
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d29fca8ae26c3bba971484be29c31871
https://doi.org/10.1016/j.bmcl.2004.01.042
https://doi.org/10.1016/j.bmcl.2004.01.042
Autor:
Arba L. Ager, Geoffrey W. Birrell, Kurt W. Saionz, Hong Ming Shieh, Gavin D. Heffernan, G. Dennis Shanks, Laura R. Jacobus, Jacek Terpinski, Peter E. Krasucki, Guy A. Schiehser, Wenyi Zhao, Michael D. Edstein, David P. Jacobus, Marina Chavchich
Publikováno v:
Antimicrobial agents and chemotherapy. 59(1)
4-( tert -Butyl)-2-(( tert -butylamino)methyl)-6-(6-(trifluoromethyl)pyridin-3-yl)-phenol (JPC-2997) is a new aminomethylphenol compound that is highly active in vitro against the chloroquine-sensitive D6, the chloroquine-resistant W2, and the multid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9093d47902841cff1f51e924c3757c33
https://pubmed.ncbi.nlm.nih.gov/25331702
https://pubmed.ncbi.nlm.nih.gov/25331702